Synthesis, Cytotoxicity and Antileishmanial Activity of Some N-(2-(indol-3-yl)ethyl)-7-chloroquinolin-4-amines

Authors

  • Elaine S. Coimbra,

    1. Departamento de Parasitologia, Microbiologia e Imunologia, Instituto de Ciências Biológicas, Universidade Federal de Juiz de Fora, Juiz de Fora, M.G. 36036-900, Brasil
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  • Rafael Carvalhaes,

    1. Departamento de Quimica, Instituto de Ciências Exatas, Universidade Federal de Juiz de Fora, Juiz de Fora, M.G. 36036-900, Brasil
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  • Richard M. Grazul,

    1. Departamento de Quimica, Instituto de Ciências Exatas, Universidade Federal de Juiz de Fora, Juiz de Fora, M.G. 36036-900, Brasil
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  • Patricia A. Machado,

    1. Departamento de Parasitologia, Microbiologia e Imunologia, Instituto de Ciências Biológicas, Universidade Federal de Juiz de Fora, Juiz de Fora, M.G. 36036-900, Brasil
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  • Marcos V. N. De Souza,

    1. FioCruz- Fundação Oswaldo Cruz, Instituto de Tecnologia em Fármacos-Far Manguinhos, Rua Sizenando Nabuco, 100, Manguinhos, Rio de Janeiro, R.J. 21041-250, Brasil
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  • Adilson D. Da Silva

    Corresponding author
    1. Departamento de Quimica, Instituto de Ciências Exatas, Universidade Federal de Juiz de Fora, Juiz de Fora, M.G. 36036-900, Brasil
      Corresponding author: A. D. Da Silva, david.silva@ufjf.edu.br
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Corresponding author: A. D. Da Silva, david.silva@ufjf.edu.br

Abstract

We report herein the condensation of 4,7-dichloroquinoline (1) with tryptamine (2) and D-tryptophan methyl ester (3). Hydrolysis of the methyl ester adduct (5) yielded the free acid (6). The compounds were evaluated in vitro for activity against four different species of Leishmania promastigote forms and for cytotoxic activity against Kb and Vero cells. Compound (5) showed good activity against the Leishmania species tested, while all three compounds displayed moderate activity in both Kb and Vero cells.

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